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DRUG CLASS:

KRAS G12V inhibitor

1m
Trial suspension • IO biomarker
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HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • TMB (Tumor Mutational Burden) • MSI (Microsatellite instability) • NTRK (Neurotrophic receptor tyrosine kinase)
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KRAS mutation • TMB-H • BRAF mutation • HER-2 amplification • ROS1 fusion • KRAS G12 • NTRK fusion
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cyclophosphamide • bendamustine • fludarabine IV
4ms
Enrollment closed
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KRAS (KRAS proto-oncogene GTPase)
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KRAS mutation • KRAS G12
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AFNT-211
6ms
A first-in-class EGFR-directed KRAS G12V selective inhibitor. (PubMed, Cancer Cell)
Using a targeted RNAi delivery platform, we achieve effective tumor silencing of KRASG12V and significant anti-tumor activity across several cancer models. Our findings represent a technological advance in oncogene targeting using RNAi and provide new biologic insights in KRAS targeting with potential implications for safety and efficacy.
Journal
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EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase)
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KRAS mutation
6ms
Enrollment open
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cyclophosphamide • fludarabine IV
7ms
NW-301 TCR-T in Patients With Advanced Solid Tumor (clinicaltrials.gov)
P1, N=44, Not yet recruiting, Peking University
New P1 trial
7ms
Identification and characterization of oncogenic KRAS G12V inhibitory peptides by phage display, molecular docking and molecular dynamic simulation. (PubMed, Comput Biol Med)
Both peptides demonstrated significant inhibition of KRAS G12V-carrying cancer cell lines (NCI-H2444 and SW620), reducing cell viability by 70-75 % at 400 μM after 48 h while showing minimal effects (20-30 % reduction) on wild-type KRAS-carrying Caco-2 cells, which is equal to DMSO diluent control. These findings provide new insights into peptide-based targeting of KRAS G12V and demonstrate the potential of using subtractive phage display for developing selective inhibitors against oncogenic mutations.
Journal
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KRAS (KRAS proto-oncogene GTPase)
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KRAS mutation • KRAS wild-type • RAS wild-type
8ms
New P1 trial
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cyclophosphamide • fludarabine IV
10ms
Enrollment closed • Enrollment change • IO biomarker
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HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • TMB (Tumor Mutational Burden) • MSI (Microsatellite instability) • NTRK (Neurotrophic receptor tyrosine kinase)
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KRAS mutation • TMB-H • BRAF mutation • HER-2 amplification • ROS1 fusion • KRAS G12 • NTRK fusion
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cyclophosphamide • bendamustine • fludarabine IV
11ms
QTX3544-201: QTX3544 in Patients With Advanced Solid Tumors With KRAS G12V Mutations (clinicaltrials.gov)
P1, N=237, Recruiting, Quanta Therapeutics | Not yet recruiting --> Recruiting
Enrollment open
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Erbitux (cetuximab)
1year
New P1 trial • Metastases
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Erbitux (cetuximab)
over1year
New P1 trial • Metastases